产品名称

CB1954

一般描述

CB1954 is a anticancer prodrug that is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent. It can be activated by NAD(P)H quinone oxidoreductase 2.

别 称

Tretazicar; 5-(aziridin-1-yl)-2,4-dinitrobenzamide   

纯 度

≥98.5%(HPLC)

CAS NO.

21919-05-1

分子式

C⁹H⁸N⁴O⁵

分子量

252.18

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25°C)

DMSO

≥45mg/ml

乙醇

Insoluble

水

Very slightly soluble

l  生物学信息

生物活性/药理作用

Tretazicar is a prodrug of a bifunctional alkylating, dinitrobenzamide derivative with antineoplastic activity. Tretazicar can be activated by the human enzyme quinone oxidoreductase 2 (NQO2) in the presence of the cosubstrate caricotamide, an analogue of the natural cosubstrate dihydronicotinamide riboside (NRH), which acts as an electron donor. The resulting active, but short-lived metabolite, dinitrobenzamide, leads to DNA replication inhibition and the induction of apoptosis in NQO2 expressing cancer cells. Due to the lack of the natural cosubstrate NRH, NQO2  is normally latent but is upregulated in certain types of tumor cells.

l  存储

存储温度

-20°C

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov